LD2-3
LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3040077-52-6
- Formel: C59H74FN11O18
- Molecular Weight:1244.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
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Topoisomerase I |
In Vitro
BGA3457 (anti-FGFR2b antibody BGAh9179 conjugated to LD2-3) (34.75 ng/mL) exhibits potent bystander killing activity against FGFR2b-negative HuTu-80-NanoLuc cells cocultured with FGFR2b-positive SNU-16 cells, with an IC50 of 34.75 ng/mL and a maximum killing potency of 90.74%[1].
BGA3457 and BGA9823 (anti-FGFR2b antibodies conjugated to LD2-3) exhibit comparable internalization activity in SNU16, SNU601-h2b, H1048-h2b, and HSC-39 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
LD2-3 (10 mg/kg; i.v.; single dose), as part of immunoconjugate BGA9823, induces complete regression of mixed FGFR2b-positive/negative gastric tumors in BALB/c nude mice[1].
LD2-3 (1-10 mg/kg; i.v.; single dose), as part of immunoconjugates BGA3457 and BGA9823, inhibits tumor growth in a FGFR2b-expressing gastric cancer xenograft model in BALB/c nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6 to 8 weeks old)[1]
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Dosage:10 mg/kg (delivered as part of immunoconjugate BGA3457)
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Administration:i.v.; single dose
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Result:Induced complete tumor regression in both 2:1 and 5:1 HSC-39:SNU-5 co-inoculation models.
Chemical Information
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CAS. Nr. 3040077-52-6
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Molecular Weight 1244.28
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Formel C59H74FN11O18
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SMILES
O=C(C=CC1=O)N1CC(NCCC(N[C@@H](CCC(NC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)CC(N)=O)=O)C(N[C@@H](C(C)C)C(N[C@@H](C)C(NCOCC(C)(C)C(N[C@@H]3C4=C5C(C(N6C5)=CC([C@](O)(C(OC7)=O)CC)=C7C6=O)=NC8=CC(F)=C(C)C(CC3)=C84)=O)=O)=O)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Neuron-Astrocyte Co-culture
Neuron-astrocyte co-culture is used to study how astrocytes regulate neuronal survival, synapse formation, dendritic morphology, neuronal activity, and disease-related neurotoxicity. Indirect “sandwich” or insert-based designs physically separate neurons and astrocytes while allowing soluble astrocyte-derived factors to affect neurons, whereas direct co-culture permits cell-contact and network-level readouts.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)